Tesamorelin (TH9507) is one of the few synthetic peptides that is approved by the FDA for human use.
It is an analog of the growth hormone-releasing hormone (GHRH) and works by activating the GHRH receptors in the pituitary gland, which stimulates the synthesis of human growth hormone (HGH).
It can be prescribed for individuals with HIV/AIDS who suffer from abnormal body fat distribution called lipodystrophy. The elevated HGH levels exert fat-burning effects on visceral adiposity and also stimulate lean body mass gain and recovery in those patients.
Due to its ability to increase the natural production of HGH and also its favorable safety profile, tesamorelin has also become a popular performance-enhancing drug (PED) among bodybuilders and athletes. However, using it without a prescription is illegal.
In the US, tesamorelin is not a controlled substance, but it is also not available over the counter (OTC), and you can obtain it legally from pharmacies only if you have a medical prescription.
Obtaining tesamorelin from sources that do not require a prescription carries a risk that you are purchasing counterfeit products that have reduced quality and potency and may be expired or even contaminated.
What is Tesamorelin?
Tesamorelin is manufactured by the Canadian company Theratechnologies and is available under the trade name Egrifta and Egrifta SV (SV = small volume).
The main difference between the two is that Egrifta SV contains double the concentration while still having the same volume after reconstitution. Thus, the patients have to subcutaneously inject a much smaller volume. This makes the injection process easier and less painful.
Tesamorelin is also illegally manufactured in the form of nasal spray. It’s unclear if these products contain the peptide because they are not a subject of any quality control, but even if they do, it’s unknown if tesamorelin can get absorbed through the nasal mucosa. It may have poor absorption through the nasal mucosa due to its large molecular weight.
What does Tesamorelin do?
Tesamorelin can stimulate the natural synthesis of HGH in individuals with preserved pituitary function, and it is much better researched compared to other GHRH mimetics.
For example, multiple clinical studies have shown that it is highly effective in reversing abnormal fat distribution in conditions such as HIV.
As a result, the FDA approved tesamorelin for therapy in patients with HIV who also suffer from lipodystrophy. Currently, this is the only FDA-approved indication for the use of tesamorelin.
Lipodystrophy is a condition that can occur in people with HIV who are undergoing antiretroviral therapy (ART), but also as a consequence of the infection itself.
It is characterized by changes in the distribution of body fat, leading to the loss of subcutaneous fat in some areas, such as the skin, and an accumulation of fat in others, such as the upper back, the abdomen, and the internal organs (visceral fat).
As a result of excessive visceral fat accumulation, HIV patients also often develop a metabolic syndrome that is associated with insulin resistance and an increased risk of heart disease.
The exact cause of the condition is unclear, but scientists suspect that neurohormonal dysregulation related to the growth hormone axis plays a role in causing these debilitating conditions.
Tesamorelin can help increase the levels of GH in these patients, which stimulates fat breakdown in the abdominal area, helps improve fat distribution, and decreases fat deposits around internal organs.
Studies report that 12 months of tesamorelin therapy can lead to an 18% reduction of visceral fat on average and is also well tolerated amongst HIV patients. Yet, it’s important to note that tesamorelin cannot lead to an increase in HGH that exceeds the physiological limits.
In comparison, therapy with high doses of injectable HGH can lead to a much higher increase in serum levels and much faster results.
Studies report that 6 mg/d of HGH can lead to a whopping 42% reduction of visceral fat in just 3 months. However, the use of such doses is also associated with a much higher risk of side effects.
Helps weight loss and reduce visceral fat
Improve muscle growth
Enhance cognitive function
How to use Tesamorelin correctly
Tesamorelin must be injected subcutaneously, and the most suitable area for the injection is the skin on the abdomen.
It’s important to choose an injection site that is at least 2 inches (5 cm) away from your belly button. Do not inject the medication into the belly button or into areas with scar tissue, bruises, reddening, infection, or irritation.
Tesamorelin comes in a 2 mg vial which must be reconstituted before use. To do so, you must use a 1″ 20-gauge needle and draw in all 0.5 ml from the vial of sterile water that is provided alongside the medication.
Then inject it into the tesamorelin vial while directing the needle towards the walls of the vial and not at the powder to avoid foaming.
You can gently roll the vial in your hands so that the powder and the water mix better, but avoid shaking it or performing any other energetic movements with the vial because it can damage the peptide.
After mixing, the solution should look clear and colorless, with no particles in it. A different syringe and a smaller needle (1/2″) are then used for the subcutaneous injection.
Once tesamorelin is reconstituted with sterile water, it must be used immediately and cannot be stored in the mixed form for later use.
Tesamorelin must be injected once daily, and you should take it at the same time every day to avoid missing a dose. However, there is no particular time of the day that will improve the effectiveness of the medication.
Furthermore, food does not interact with tesamorelin injections.
What is a proper Tesamorelin dosage?
The standard dosage for tesamorelin therapy in HIV-associated lipodystrophy is 2 mg taken once daily. The medication is available in two strengths – Egrifta, which is 1 mg per vial, and Egrifta SV, which is 2 mg per vial.
You should not take double the dosage to compensate for any missed doses. Instead, make sure to simply go back to your regular injection schedule.
Tesamorelin has also been tested for weight loss in healthy obese individuals, and the dosage was still 2mg per day.
Tesamorelin was successful in reducing visceral fat in healthy obese individuals, but it’s important to note that it did not affect subcutaneous body fat or body weight.
How can you get Tesamorelin?
Tesamorelin is a prescription-only medication which means that you must have a medical prescription to obtain the drug from a legal US pharmacy.
A doctor will offer you a tesamorelin prescription if you meet the indications for the therapy, such as having excess abdominal fat due to HIV-associated lipodystrophy.
Yet, tesamorelin is not a controlled medication, and some doctors may consider prescribing it off-label.
It’s important to note that tesamorelin is quite expensive, and 2 mg of tesamorelin per day for a 30-day supply costs over $7000.
One of the reasons for its high price is that the medication is still under patent by its original manufacturer – Theratechnologies. Thus, it is available only under the brand name Egrifta, and there are no generic options available.
Other therapeutic options for the management of HIV-associated lipodystrophy include changing some of your HIV medications with new ones that are less likely to cause the condition, as well as lifestyle changes.
A combination of muscle-building exercises and a healthy diet can help prevent the deposition of abdominal fat. Surgery can also be performed to remove any abnormal fat deposits and insert implants in areas of lipoatrophy.
Your doctor may also prescribe you metformin and statins, if you have high insulin resistance, elevated blood sugar or cholesterol levels due to excess abdominal fat.
Furthermore, your doctor is not going to offer you a tesamorelin prescription or therapy if you have any contraindications, such as a damaged pituitary gland, active malignancy, known hypersensitivity to tesamorelin, or if you are pregnant. Modifying visceral adipose tissue offers no benefit in a pregnant woman and may harm the baby.
What results to expect from Tesamorelin?
As previously noted, studies show that long-term tesamorelin therapy is highly effective for reducing visceral fat in patients with lipodystrophy. The majority of trials report a 10-20% reduction in organ fat after 3-12 months of tesamorelin treatment compared to before the therapy.
The researchers report that the first effects of the therapy can occur as soon as 12 weeks of daily injections, and taking 2 mg tesamorelin a day led to an 11.3% higher reduction in visceral fat compared to a placebo.
However, none of these studies report a significant change in the levels of subcutaneous fat or body weight. Therefore, tesamorelin is not indicated for weight loss management as it has a weight-neutral effect.
This is why tesamorelin may not be that effective for fat loss in athletes such as bodybuilders, at least in the doses reported by scientific research.
Benefits of Tesamorelin
Tesamorelin therapy has the following proven and potential benefits:
- reducing visceral fat
- reducing muscle wasting
- increase in lean body mass
- increases HGH and IGF-1 levels
- may improve cognitive function
Most studies in HIV patients also report a small but statistically significant increase in lean body mass, increased IGF-1 levels, and reduced muscle wasting.
According to a clinical trial, the administration of tesamorelin for 20 weeks may also result in better cognitive function in healthy older adults and elderly individuals with mild cognitive impairment.
The study also indicated that the levels of GABA increased in all three brain regions, NAAG levels increased in the frontal cortex, and MI levels decreased in the posterior cingulate after the 20-week treatment with tesamorelin.
The authors of the study proposed that the beneficial effects of tesamorelin on the inhibitory neurotransmitters GABA and NAAG may have contributed to the observed improvement in cognitive function.
Studies do not report any direct effect of tesamorelin on sex hormones such as testosterone, libido, and sleep. On the other hand, PT-141(bremelanotide) has a positive impact on erectile function, sexual desire, and overall sexual satisfaction in men and women.
Yet, tesamorelin may provide indirect benefits for testosterone and libido in men by reducing visceral fat and improving metabolic health. That’s because visceral adiposity can suppress the normal function of the hypothalamic–pituitary–testicular axis.
Furthermore, tesamorelin has uncertain benefits regarding muscle growth. Most studies do not report significant muscle growth during therapy, but the peptide may result in increased muscle density among HIV patients.
Side effects of Tesamorelin
The most common side effects of tesamorelin include local reactions at the injection site, such as:
They can occur due to improper administration of the medication. Some patients may also develop edema-related reactions such as joint and leg pain, swollen legs, and carpal tunnel syndrome.
Rare side effects include facial flushing, palpitations, and hypersensitivity reactions such as rashes
Reduced glucose tolerance and hyperglycemia are extremely rare. Such reactions may occur due to the sudden increase in HGH levels at the start of tesamorelin therapy.
These side effects are transitory as it takes time for patients to adapt to the increase in HGH levels after starting tesamorelin therapy.